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Microbiology

Supramolecular Nanorods of (N-Methylpyridyl) Porphyrin With Captisol: Effective Photosensitizer for Anti-bacterial and Anti-tumor Activitie

5 | Aug 05 2019

Khurana R et al. indicatted that all these synergistic effects of supramolecular nanorods of Captisol-TMPyP complex make the system an effective photosensitizer and a superior antibacterial and antitumor agent. [Read the Full Post]

Associated-Extraction Efficiency of Six Cyclodextrins on Various Flavonoids in Puerariae Lobatae Radix

7 | Jul 05 2019

Feng T et al. indicated that CDs, especially SBE-β-CD, have a promising application for the associated-extraction of flavonoids from PLR. [Read the Full Post]

In Vitro Activity of Sitafloxacin and Additional Newer Generation Fluoroquinolones Against Ciprofloxacin-Resistant Neisseria gonorrhoeae Isolates

10 | Jul 01 2019

Hamasuna R et al. indicated that sitafloxacin should not be considered for empirical first-line monotherapy of gonorrhea. However, sitafloxacin could be valuable in a dual antimicrobial therapy and for cases with ceftriaxone resistance or allergy. [Read the Full Post]

Raltegravir (MK-0518): an integrase inhibitor for the treatment of HIV-1

18 | Jun 20 2019

Evering TH et al. indicated it has demonstrated a favorable side-effect profile in treatment-naive and -experienced patients and a subset of heavy treatment-experienced patients have been able a achieve virologic suppression with raltegravir as part of combination therapy despite limited treatment options. [Read the Full Post]

Puromycin reaction for the A site-bound peptidyl-tRNA

19 | Jun 16 2019

Semenkov Yu et al. indicated that the transpeptidation reaction per se triggers conformational changes in the ribosomal complex bringing the 3'-end of a newly synthesized peptidyl-tRNA nearer to the peptidyl-site of the peptidyltransferase center. This is detected functionally as the ability of such an A site bound peptidyl-tRNA to react with puromycin. This reaction is highly pronounced at elevated (25 degrees C) temperature but can be hardly detected at 0 degrees C. [Read the Full Post]

In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor

31 | May 28 2019

Kobayashi M et al. demonstrated that S/GSK1349572 would be classified as a next-generation drug in the integrase inhibitor class, with a resistance profile markedly different from that of first-generation integrase inhibitors. [Read the Full Post]

Coformulated bictegravir, emtricitabine, and tenofovir alafenamide versus dolutegravir with emtricitabine and tenofovir alafenamide, for initial treatment of HIV-1 infection (GS-US-380-1490): a randomised, double-blind, multicentre, phase 3, non-inferiority trial

32 | May 08 2019

Sax PE et al. indicated at 48 weeks, virological suppression with the bictegravir regimen was achieved and was non-inferior to the dolutegravir regimen in previously untreated adults. There was no emergent resistance to either regimen. The fixed-dose combination of bictegravir, emtricitabine, and tenofovir alafenamide was safe and well tolerated compared with the dolutegravir regimen. [Read the Full Post]

Is maraviroc useful in multiple sclerosis patients with natalizumab-related progressive multifocal leukoencephalopathy

80 | Apr 15 2019

Scarpazza C et al. showed that maraviroc did not show any clear effect in modulating the clinical course of PML preventing IRIS. Moreover, once PML-IRIS emerged, the clinical stabilization was achieved only with the use of corticosteroids. Thus, the use of maraviroc should be regarded with extreme caution due the potential adverse events associated with its use. [Read the Full Post]

MK2206 enhances the cytocidal effects of bufalin in multiple myeloma by inhibiting the AKT/mTOR pathway

86 | Jan 11 2019

Xiang RF et al. suggested that MK2206 significantly enhanced the cytocidal effects of bufalin in MM cells, regardless of the sensitivity to bortezomib, via the inhibition of the AKT/mTOR pathway. The study provided the basis of a promising treatment approach for MM. [Read the Full Post]

Micafungin-Induced Suicidal Erythrocyte Death

136 | Nov 14 2018

Peter T et al. showed effect of Micafungin on annexin-V-binding was not significantly modified by removal of extracellular Ca2+, by PKC inhibitor staurosporine (1 µM), p38 kinase inhibitor SB203580 (2 µM), casein kinase 1α inhibitor D4476 (10 µM) or pancaspase inhibitor zVAD (10 µM). [Read the Full Post]

Smac mimetic with TNF-α targets Pim-1 isoforms and reactive oxygen species production to abrogate transformation from blebbishields

349 | Oct 29 2018

Jinesh GG et al. demonstrated that Smac mimetic in combination with TNF-α is an ideal candidate to target Pim-1 expression, inhibit ROS production and to block transformation from blebbishields. [Read the Full Post]

Antimicrobial susceptibility testing of rapidly growing mycobacteria isolated in Japan

179 | Oct 28 2018

Hatakeyama S et al. demonstrated the importance of correct identification and antimicrobial susceptibility testing, including the testing of potential new agents, in the management of RGM infections. [Read the Full Post]

Tumor Necrosis Factor Inhibits Spread of Hepatitis C Virus Among Liver Cells, Independent From Interferons

201 | Oct 10 2018

Laidlaw SM et al. found TNF to have antiviral effects independently of, as well as in combination with, IFNs. TNF inhibits HCV infection despite increased HCV envelope glycoprotein-mediated infection of liver cells. These findings contradict those from other studies, which have reported that TNF blocks signal transduction in response to IFNs. The destructive inflammatory effects of TNF must be considered along with its antiviral effects. [Read the Full Post]

PTC725, an NS4B-Targeting Compound, Inhibits a Hepatitis C Virus Genotype 3 Replicon, as Predicted by Genome Sequence Analysis and Determined Experimentally

0 | Oct 09 2018

Graci JD et al. identified previously unreported amino acid substitutions selected by PTC725 treatment which further demonstrate that these compounds target the NS4B first transmembrane region. [Read the Full Post]

Inhibition of Histone Deacetylase Activity Aggravates Coxsackievirus B3-Induced Myocarditis by Promoting Viral Replication and Myocardial Apoptosis

190 | Sep 08 2018

Zhou L et al. found inhibition of HDAC activity enhanced myocardial autophagosome formation, which led to the elevated CVB3 viral replication and ensuing increased myocardial apoptosis. [Read the Full Post]

Hepatitis C Virus NS4B Can Suppress STING Accumulation To Evade Innate Immune Responses

477 | Aug 13 2018

Yi G et al. showed that 2a/JFH1 NS4B has an additional mechanism to evade STING signaling through suppressing STING accumulation. [Read the Full Post]

A profiling study of a newly developed HCVcc strain PR63cc's sensitivity to direct-acting antivirals

467 | Aug 12 2018

Tao W et al. showed that PR63cc was more resistant than JFH1 to the asunaprevir/daclatasvir combination treatment. In summary, our study systemically analyzed the DAA sensitivity of a new HCVcc strain and identified critical RAVs. These results are not only important for monitoring the emergence of drug-resistant mutations of current DAA therapies, but also valuable for developing next-generation DAAs. [Read the Full Post]

A simple and cost-saving phenotypic drug susceptibility testing of HIV-1

632 | Jul 05 2018

Weng Y et al. provided a useful tool for interpreting meaningful genotypic mutations and guiding tailored antiviral treatment of HIV/AIDS in clinical practice. [Read the Full Post]

Dissecting the molecular mechanisms that impair stress granule formation in aging cells

460 | Jul 04 2018

Moujaber O et al. demonstrated that the loss of CReP correlated with the aging-related hyperphosphorylation of eIF2α. Together, we have identified significant changes in the stress response of aging cells and provide mechanistic insights. Based on our work, we propose that the decline in SG formation can provide a new biomarker to evaluate cellular aging. [Read the Full Post]

HMGB1-mediated autophagy decreases sensitivity to oxymatrine in SW982 human synovial sarcoma cells

525 | May 13 2018

Cai Y et al. showed that combining OMT with an inhibitor of autophagy or HMGB1 may make OMT more effective in the treatment of human synovial sarcoma. [Read the Full Post]

In silico prediction and in vitro and in vivo validation of acaricide fluazuron as a potential inhibitor of FGFR3 and a candidate anticancer drug for bladder carcinoma

442 | Apr 20 2018

Ke K et al. suggested for the first time that fluazuron is a potential inhibitor of FGFR3 and a candidate anticancer drug for the treatment of BC. [Read the Full Post]

Susceptibility of porcine endogenous retrovirus to anti-retroviral inhibitors

326 | Apr 09 2018

Argaw T et al. indicated that some of the licensed anti-retroviral drugs may be useful for controlling PERV infection. However, the efficacy at nanomolar concentrations put forward integrase inhibitors as a drug that has the potential to be useful in the event that xenotransplantation recipients have evidence of PERV transmission and replication. [Read the Full Post]

In Vitro Antibacterial Activity of Rhodanine Derivatives against Pathogenic Clinical Isolates

672 | Mar 08 2018

AbdelKhalek A et al. suggested that certain rhodanine compounds may have potential use for the treatment of several multidrug-resistant Gram-positive bacterial infections. [Read the Full Post]

Membrane Interactions of Natural Cyclic Lipodepsipeptides of the Viscosin Group.

461 | Feb 18 2018

Geudens N, et al. found that the CLPs interact both with the polar heads and aliphatic tails of model membrane systems, altering bilayer fluidity, while cholesterol reduces CLP insertion depth. [Read the Full Post]

Antibacterial activity and mechanism of action of auranofin against multi-drug resistant bacterial pathogens

635 | Feb 03 2018

Thangamani S et al. provided valuable evidence that auranofin has significant promise to be repurposed as a novel antibacterial for treatment of invasive bacterial infections. [Read the Full Post]

New insights into the interaction between pyrrolyl diketoacids and HIV-1 integrase active site and comparison with RNase H

534 | Jan 11 2018

Corona A et al. provided new structural information to modulate IN and RNase H inhibitory activities for development of dual-acting anti-HIV agents. [Read the Full Post]

Repurposing auranofin for the treatment of cutaneous staphylococcal infections

626 | Jan 06 2018

Thangamani S et al. supported that auranofin has potential to be repurposed as a topical antimicrobial agent for the treatment of staphylococcal skin and wound infections. [Read the Full Post]

PTC725, an NS4B-Targeting Compound, Inhibits a Hepatitis C Virus Genotype 3 Replicon, as Predicted by Genome Sequence Analysis and Determined Experimentally.

718 | Dec 29 2017

Graci JD et al. identified previously unreported amino acid substitutions selected by PTC725 treatment which further demonstrate that these compounds target the NS4B first transmembrane region. [Read the Full Post]

Anidulafungin-Induced Suicidal Erythrocyte Death

0 | Nov 01 2017

Anidulafungin triggers hemolysis and eryptosis with cell shrinkage and phospholipid scrambling of the erythrocyte cell membrane, an effect in part due to Ca2+ entry and activation of p38 kinase. [Read the Full Post]

Cancer-associated fibroblasts promote hepatocellular carcinoma metastasis through chemokine-activated hedgehog and TGF-β pathways

893 | Oct 28 2017

Liu J et al. found that CAF-secreted CCL2, CCL5, CCL7 and CXCL16 promote HCC metastasis through the coordinate activation of Hh and TGF-β pathways in HCC cells. [Read the Full Post]

Ebola VP40 in Exosomes Can Cause Immune Cell Dysfunction

634 | Sep 24 2017

Dosch JS et al. suggested that the use of drugs such as Oxytetracycline to modulate the levels of exosomes exiting EBOV-infected cells may be able to prevent the devastation of the adaptive immune system and allow for an improved rate of survival. [Read the Full Post]

Cancer stem cell marker phenotypes are reversible and functionally homogeneous in a preclinical model of pancreatic cancer

844 | Sep 24 2017

Dosch JS, et al. showed that the hierarchical organization of CSCs in human disease is not recapitulated in a commonly used mouse model of pancreatic cancer and therefore provide a new view of the phenotypic and functional heterogeneity of tumor cells. [Read the Full Post]

Antiviral activity of micafungin against enterovirus 71

0 | Aug 05 2017

Kim C et al. identified micafungin, an echinocandin antifungal drug, as a novel inhibitor of EV71. [Read the Full Post]

Cryo-EM reveals a novel octameric integrase structure for betaretroviral intasome function

841 | Jun 17 2017

Ballandras-Colas A et al. revealed a novel octameric integrase structure for betaretroviral intasome function. [Read the Full Post]

Selectivity for strand-transfer over 3'-processing and susceptibility to clinical resistance of HIV-1 integrase inhibitors are driven by key enzyme-DNA interactions in the active site

822 | May 13 2017

Métifiot M et al. indicated that the conserved residue Q146 in the flexible loop of HIV-1 integrase is critical for productive viral DNA binding through specific contacts with the virus DNA ends in the 3'-processing and ST reactions. [Read the Full Post]

CD4+ T cell–dependent and –independent cytokine-chemokine network changes in the immune responses of HIV-infected individuals

2180 | Mar 20 2017

Arnold KB et al identified a critical deficiency in NK cell responses of HIV-infected individuals, independent of CD4(+) T cell depletion, which directs secreted profiles. Our findings illustrate a broad approach for identifying key disease-associated nodes in a multicellular, multivariate signaling network. [Read the Full Post]

Solitary inhibition of the breast cancer resistance protein (BCRP) efflux transporter results in a clinically significant drug-drug interaction with rosuvastatin by causing up to a two-fold increase in statin exposure

1786 | Feb 25 2017

Elsby R, et al.'s result shows that solitary inhibition of the intestinal BCRP transporter can result in clinically significant DDIs with rosuvastatin, causing up to a maximum 2-fold increase in exposure, which may warrant statin dose adjustment in clinical practice [Read the Full Post]

Understanding the molecular mechanism of host-based statin resistance in hepatitis C virus replicon containing cells

1616 | Jan 28 2017

Delang L et al. demonstrated that statin resistance in HCV replicon containing hepatoma cells is conferred by changes in the cellular environment. [Read the Full Post]

CD4+ T cell–dependent and –independent cytokine-chemokine network changes in the immune responses of HIV-infected individuals

2390 | Jan 24 2017

Arnold KB, et al. identified a critical deficiency in NK cell responses of HIV-infected individuals, independent of CD4(+) T cell depletion, which directs secreted profiles. Our findings illustrate a broad approach for identifying key disease-associated nodes in a multicellular, multivariate signaling network. [Read the Full Post]

Cancer-associated fibroblasts promote hepatocellular carcinoma metastasis through chemokine-activated hedgehog and TGF-β pathways

2989 | Nov 10 2016

Liu J et al. found thatCAF-secreted CCL2, CCL5, CCL7 and CXCL16 promote HCC metastasis through the coordinate activation of Hh and TGF-β pathways in HCC cells. [Read the Full Post]

Linking IFNα to apolipoprotein A-I provides a novel therapy of chronic hepadnavirus infection

1856 | Mar 25 2015

Berrondo et al. demonstrated a molecule called InterApo (IA) with IFNα links to apolipoprotein A-I, has antiviral and immunostimulatory activities and lacks IFNα-induced hematological toxicity. In this study, they further explore the safety of IA for chronic HBV infection. [Read the Full Post]

The inhibitor of CCR5 block metastasis of v-Src oncogene-transformed prostate cancer

2551 | Dec 11 2014

Sicoli et al. identified CCR5 signaling activation is important for v-Src oncogene-transformed prostate cancer metastasis, and it antagonist can attenuate the burden. [Read the Full Post]

Semen suppresses antiviral activities of microbicides against HIV

2322 | Nov 25 2014

Zirafi et al. reported that microbicides, which can target HIV components, showed ineffective in the presence of semen. [Read the Full Post]

Maraviroc is an antiretroviral drug in the CCR5 receptor antagonist class

2880 | Mar 13 2014

Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM, respectively. [Read the Full Post]

Maraviroc is an antiretroviral drug in the CCR5

0 | Jan 21 2014

Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM, respectively. [Read the Full Post]

Maraviroc is an antiretroviral drug in the CCR5 receptor

2890 | Dec 29 2013

Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM, respectively. [Read the Full Post]

Maraviroc is an antiretroviral drug in the CCR5

2969 | Nov 20 2013

Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM, respectively. [Read the Full Post]

BMS 790052 is the most potent hepatitis C virus inhibitor

3694 | Nov 13 2013

BMS-790052 is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3. [Read the Full Post]

Vicriviroci s a pyrimidine CCR5 entry inhibitor of HIV1

2914 | Jul 20 2013

Vicriviroc binds with higher affinity to CCR5 versus SCH-C (SCH-351125) in competition binding assays with Ki value of 0.8 nM versus 2.6 nM. [Read the Full Post]

Telaprevir is an associate of a class of antiviral drugs

3843 | Mar 21 2013

Telaprevir is an associate of a class of antiviral drugs called protease inhibitors. Especially, telaprevir prevents the hepatitis C viral enzyme NS3.4A serine protease. Telaprevir is just indicated for use against hepatitis d genotype 1 viral infections and hasnt been which can have an impact on or being protected when employed for other genotypes of the herpes virus. The standard therapy of ribavirin and pegylated interferon is less successful on genotype 1 and a welcome addition is offered by telaprevir to the treatment of this genotype. [Read the Full Post]

Raltegravir is an antiretroviral drug produced by Merck and Co

2513 | Dec 12 2012

Epigenetic marks play a major role in the control of cell fate during mammalian development. Among these, the most studied so far is lysine acetylation, a posttranslational modification of histones which inactivates the positive Raltegravir charge of lysines. [Read the Full Post]

Maraviroc provide a mechanism to adjust the properties

2944 | Nov 28 2012

Our data also indicate that activity of AurA IFT88 localization affected during disassembly and suggest the integrity of t the Maraviroc is important for the process of removing animals, as in Chlamydomonas. [Read the Full Post]

Telaprevir has very poor penetration of the blood brain

4910 | Nov 15 2012

The principal metabolic fate of loperamide in humans involves oxidative N dealkylation to N demethyl loperamide as the principal metabolite. In human liver microsomes, cytochrome P450 3A4 appears to be the major isozyme responsible for loperamide metabolism, with minor contributions from CYP2B6 [Read the Full Post]

BMS-790052 A Tr droplets With twice as many cells pressed

3643 | Oct 23 2012

BMS-790052 A Tr droplets With twice as many cells pressed agA Tr droplets, With twice as many cells pressed against the heart tee h Here cAMP concentration against each other, the proportion of droplets tears reported a positive response [Read the Full Post]

RALTEGRAVIR- AN INTEGRASE INHIBITOR

3118 | Jul 30 2012

HIV-I AND INTEGRASE HIV one of the most tricky viruses on earth that cause immunodeficiency in humans is being studied allot. It is responsible for a deathly disease known AIDS which is a focus of attention of many researchers since last decades. Due to its wide spread and occurrence throughout the world has compelled the scientists to look for a drug that may effectively cure the disease. HIV contains different types of enzymes and genes that help it to utilize the genes and proteins of its host. The most important among all is the integrase enzyme that helps it in integration of its genome into that of the host. Integrase has been an attractive target for the devising a therapy against the disease. A lot of research is being done on integrase inhibitors and several integrase inhibitors have been discovered by high throughput screening that prevent the integration of genome of virus into that of the host hence preventing the proliferation of the host cell. These inhibitors have shown efficacious results when used against HIV-I. One of the examples of such inhibitors is Raltegravir integrase inhibitor. This drug is first of such inhibitors to get FDA approval and is a blessing for the patients of HIV. [Read the Full Post]

RALTEGRAVIR- FAMOUS INTEGRASE INHIBITOR

3399 | Jun 03 2012

INTEGRASE IN CASE OF HIV-1 The most deathly disease on earth, HIV-I, is being researched and studied a lot to find out an effective therapy against it. This virus contains some genes for enzymes/proteins and utilizes some others from the host cells. The enzyme in HIV that helps the virus to integrate its genome into host cell/genome is named as Integrase and gets replicated there. To search for the [roper treatment the first thing that must be keep in mind is resistance development by the mutation of their genes during replication, so it is the need of hour that the research about treatment of cancer must go on further and should be regularly updated. To inhibit their enzymatic activity is an attractive approach. The inhibitors for integrase enzyme have been developed and they inhibit the process of integration of viral genome into the host genome hence prevent its proliferation in the hosting cell. A huge wave of research is going on HIV-I regarding integrase inhibitors that offer promising results against HIV-I virus. Raltegravir integrase inhibitor is such an inhibitor that inhibits the integrase enzyme and it is the first inhibitor to get approved from FDA and its discovery is no doubt considered to be a great blessing. [Read the Full Post]

RALTEGRAVIR- AN INTEGRASE INHIBITOR

3515 | Apr 27 2012

INTEGRASE AND HIV-1 HIV-I, one of the deathly diseases present on earth, is being researched a lot in order to find an efficacious therapy against it. The virus contains some of the genes for proteins/enzymes and utilizes some from the host. Integrase is one of the enzymes present in virus that helps it to integrate its genome into the host genome and get itself replicated there. In order to search for the treatment, first thing that is kept in mind is the development of resistance by getting their genes mutated during replication, therefore it is need of the hour that research on the treatment against cancer must go on and should be updated. Inhibiting the enzymatic activity is one of the approaches. Inhibitors of integrase have also been developed that inhibit the integration of genome of the virus into that of the host and therefore prevent it to proliferate inside the host cell. A lot of research is going on HIV-I in the area of integrase inhibitors which offer new promises in for therapy against HIV-I. Raltegravir integrase inhibitor is one of such inhibitors and the first one to get approval from FDA and the discovery of which is considered a blessing. [Read the Full Post]

RALTEGRAVIR: A POTENT INTEGRASE INHIBITOR

2464 | Apr 01 2012

INTRODUCTION TO HIV-1 AND ITS TREATMENT: HIV-1 is amongst the most destructive viruses and its treatment regime always in a need of more and novel methods to treat this virus because any of the new drugs gives a short time benefit as the virus get resistant against that drug, therefore any of the effective and newly introduced drug is welcomed by the medical practitioners. In order to integrate the genome of virus it needs integrase enzyme, thus inhibitors to this enzyme are potential candidates to inhibit the viral replication inside host cells. For the development and discovery of these inhibitors a lot of work is being done for integrase inhibitors of HIV-1 these inhibitors are also offering new hopes for HIV-1 drugs. Raltegravir integrase inhibitor, first FDA approved HIV integrase inhibitor and the discovery of this inhibitor was much valued. [Read the Full Post]